Cardiovascular disease is one of the leading causes of death in the United States and most European countries. It is estimated that over 70 million people in the United States alone suffer from a cardiovascular disease or disorder including but not limited to high blood pressure, coronary heart disease, dislipidemia, congestive heart failure and stroke.
At high doses (e.g. >1500 mg) niacin is a potent lipid lowering drug with the ability to lower very low density and low density lipoprotein particles and increase high density lipoprotein cholesterol-C (HDL-C). However, at these doses, niacin causes vascular-cutaneous flushing mediated by prostaglandin D2 and seriously limits patient compliance and thus effectiveness. At lower doses (e.g. <1500 mg/day) niacin only increases HDL-C without lowering very low density and low density lipoprotein particles. Extended- and sustained-release forms of niacin have been developed and can reduce (but not eliminate) flushing, but can also cause liver toxicity, gastrointestinal upset, nausea, diarrhea, sexual dysfunction and fatigue. These side effects significantly limit the use of niacin therapy.